Chalcogen Bonded Directly To Ring Carbon Of The Five-membered Hetero Ring Patents (Class 514/418)
  • Patent number: 6103752
    Abstract: Compounds of formula (I) ##STR1## wherein R and R.sup.1 are hydrogen, C.sub.1-4 alkyl or are linked to form a ring,A is a cycloalkyl or alkyl-cycloalkyl group,n is an integer from 0 to 3,W is an optionally substituted 5- or 6-membered heterocyclic ring; or W is an optionally substituted aryl, heteroaryl, aryloxy or thiophenoxy group; orW is a group --SO.sub.2 NR.sup.6 R.sup.7 --NHC(O)R.sup.6 R.sup.7 or --C(O)NHR.sup.6 R.sup.7 ;are useful in treating clinical conditions for which a "5-HT.sub.1 -like" receptor agonist is indicated.
    Type: Grant
    Filed: February 23, 1999
    Date of Patent: August 15, 2000
    Assignee: Glaxo Wellcome Inc.
    Inventors: Robert Charles Glen, David Lawrence Selwood, Graeme Richard Martin, Christopher James Foster
  • Patent number: 6090839
    Abstract: The instant invention is concerned with aryl and heteroaryl oxyacetic acid type compounds which are useful antidiabetic compounds. Compositions and methods for the use of the compounds in the treatment of diabetes and related diseases and for lowering triglyceride levels are also disclosed.
    Type: Grant
    Filed: December 19, 1997
    Date of Patent: July 18, 2000
    Assignee: Merck & Co., Inc.
    Inventors: Alan D. Adams, Derek Von Langen, Richard L. Tolman, Hiroo Koyama
  • Patent number: 6090818
    Abstract: The invention relates to compounds with formula (I), a process for their preparation and pharmaceutical compositions containing them.
    Type: Grant
    Filed: June 14, 1999
    Date of Patent: July 18, 2000
    Assignee: Sanofi-Synthelabo
    Inventors: Loic Foulon, Claudine Serradeil-Le Gal, Gerard Valette
  • Patent number: 6083515
    Abstract: Nonsteroidal antiinflammatory drugs which have been substituted with a nitrogen monoxide group; compositions comprising (i) a nonsteroidal antiinflammatory drug, which can optionally be substituted with a nitrogen monoxide group and (ii) a compound that directly donates, transfers or releases a nitrogen monoxide group (preferably as a charged species, particularly nitrosonium); and methods of treatment of inflammation, pain, gastrointestinal lesions and/or fever using the compositions are disclosed. The compounds and compositions protect against the gastrointestinal, renal and other toxicities that are otherwise induced by nonsteroidal antiinflammatory drugs.
    Type: Grant
    Filed: January 22, 1999
    Date of Patent: July 4, 2000
    Assignee: NitroMed, Inc.
    Inventors: David S. Garvey, L. Gordon Letts, H. Burt Renfroe, Sang William Tam
  • Patent number: 6075044
    Abstract: The use of certain heterocyclic derivatives for treating parasitic protozoa infections in mammals, in particular bovine trichomoniasis and giardiasis, is disclosed.
    Type: Grant
    Filed: July 17, 1998
    Date of Patent: June 13, 2000
    Assignee: The Regents of the University of California
    Inventors: Ching C. Wang, John Somoza, Jon P. Page, Ronaldus Marcellus Alphonsus Knegtel, Irwin D. Kuntz, Connie M. Oshiro, A. Geoffrey Skillman
  • Patent number: 6071949
    Abstract: The present method provides a method for treating an epithelial cell-derived cancer in a subject in need of such treatment which comprises administering to the subject an amount of a 5-lipoxygenase inhibitor or derivative thereof effective to treat the epithelial cell-derived cancer. The present invention also provides a method for preventing an epithelial cell-derived cancer in a subject in need of such prevention which comprises administering to the subject an amount of a 5-lipoxygenase inhibitor effective to prevent the epithelial cell-derived cancer. Suitable 5-lipoxygenase inhibitors useful for the methods of the present invention preferably include 2-(12-Hydroxydodeca-5,10-dinyl)-3,5,6-trimethyl-1,4-benzoquinone and derivatives thereof; Nordihydroguaiaretic acid and derivatives; and 3-[1-(4-chlorobenzyl)-3-t-butyl-thio-t-isopropyl-indol-2-yl]-2-2-dimethylp ropanoic acid and derivatives thereof.
    Type: Grant
    Filed: December 3, 1996
    Date of Patent: June 6, 2000
    Assignee: The United States of America as represented by the Department of Health and Human Services
    Inventors: James L. Mulshine, Marti Jett
  • Patent number: 6069164
    Abstract: A method for treating circadian rhythm phase disorders is described. The invention provides methods to specifically advance or delay the phase of certain circadian rhythms in humans. The disclosed methods relate to the administration of melatonin at times determined with relation to the time of dim light endogenous melatonin onset. Embodiments capable of alleviating the effects of jet lag, winter depression and shiftwork sleep disturbance are provided.
    Type: Grant
    Filed: January 6, 1997
    Date of Patent: May 30, 2000
    Assignee: Oregon Health Sciences University
    Inventors: Alfred J. Lewy, Robert L. Sack
  • Patent number: 6066663
    Abstract: The invention relates to derivatives of general formula I ##STR1## The invention also relates to pharmaceutical and cosmetic compositions comprising derivatives of general formula I.
    Type: Grant
    Filed: August 11, 1998
    Date of Patent: May 23, 2000
    Assignees: CEMAF, Laboratories Besins-Iscovesco S.A.
    Inventors: Jean-Bernard Fourtillan, Marianne Fourtillan, Jean-Claude Jacquesy, Marie-Paule Jouannetaud, Bruno Violeau, Omar Karam
  • Patent number: 6063806
    Abstract: A heterocyclic derivative of the formula (I) ##STR1## wherein each symbol is as defined in the specification, and pharmaceutically acceptable salts thereof. The compound (I) of the present invention and pharmaceutically acceptable salts thereof exhibit superior ACAT inhibitory activity and lipoperoxidation inhibitory activity in mammals, and are useful as ACAT inhibitors and lipoperoxidation inhibitors. Specifically, they are useful for the prophylaxis and treatment of arteriosclerosis, hyperlipemia, arteriosclerosis in diabetes, and cerebrovascular and cardiovascular ischemic diseases.
    Type: Grant
    Filed: April 3, 1998
    Date of Patent: May 16, 2000
    Assignee: Kyoto Pharmaceutical Industries, Ltd.
    Inventors: Shoji Kamiya, Hiroaki Shirahase, Hiroshi Matsui, Shohei Nakamura, Katsuo Wada
  • Patent number: 6060500
    Abstract: This invention relates to a method for inhibiting bome resorption in a patient with periodotal disease by administering 3-[1-(4-chlorolbenzyl)-3-t-butyl-thio-t-isopropylindol-2-yl]-2,2dimethylpr opanoic acid.
    Type: Grant
    Filed: December 27, 1996
    Date of Patent: May 9, 2000
    Assignee: Board of Regents, The University of Texas System
    Inventors: Lynda F. Bonewald, G.R. Mundy, Wolf E. Gallwitz
  • Patent number: 6051593
    Abstract: The present invention relates to novel 3-(cycloalkanoheteroarylidenyl)-2-indolinone compounds and physiologically acceptable salts and prodrugs thereof which are expected to modulate the activity of protein tyrosine kinases and therefore to be useful in the prevention and treatment of protein tyrosine kinase related cellular disorders such as cancer.
    Type: Grant
    Filed: June 19, 1998
    Date of Patent: April 18, 2000
    Assignee: Sugen, Inc.
    Inventors: Peng Cho Tang, Li Sun, Gerald McMahon
  • Patent number: 6028085
    Abstract: Prodrugs of 5HT.sub.
    Type: Grant
    Filed: September 30, 1998
    Date of Patent: February 22, 2000
    Assignee: SmithKline Beecham plc
    Inventor: Steven Mark Bromidge
  • Patent number: 6025369
    Abstract: The present invention relates to the novel finding that homocysteine affects the initiation and/or progress of atherosclerosis via a receptor-mediated growth factor effect on vascular smooth muscle cells. This growth factor effect can be inhibited by N-methyl-D-aspartate antagonists via a unique receptor that is in the NMDA receptor family. Through the use of cloning and other procedures, this homocysteine receptor can be characterized in order to develop novel pharmacologic strategies that the address the receptor for the prevention and treatment of atherosclerosis.
    Type: Grant
    Filed: May 2, 1997
    Date of Patent: February 15, 2000
    Assignee: The Board of Regents of the University Nebraska
    Inventors: Thomas H. Rosenquist, Daniel T. Monaghan, Preston F. Gadson, Vincent J. Andaloro
  • Patent number: 6011045
    Abstract: The present invention relates to compounds of the formula IA--B--D--E--F--G (I)in which A, B, D, E, F and G have the meanings given in the patent claims, to their preparation and to their use as medicaments. The compounds of the invention are used as vitronectin receptor antagonists and as inhibitors of bone resorption.
    Type: Grant
    Filed: December 22, 1997
    Date of Patent: January 4, 2000
    Assignees: Hoechst Aktiengesellschaft, Genentech, Inc.
    Inventors: Volkmar Wehner, Hans Ulrich Stilz, Anuschirwan Peyman, Jochen Knolle, Jean-Marie Ruxer, Denis Carniato, Jean-Michel Lefrancois, Thomas Richard Gadek, Robert McDowell
  • Patent number: 6001866
    Abstract: This invention provides a method for treating or preventing inflammation or atherosclerosis in mammals comprising administering an effective amount of a 15-LO inhibitor of Formula I: ##STR1## wherein: R.sup.1 is hydrogen or C.sub.1 -C.sub.6 alkyl;R.sup.2, R.sup.3, R.sup.4, and R.sup.5 independently are hydrogen, C.sub.1 -C.sub.6 alkyl, nitro, halo, CN, OR.sup.6, NR.sup.6 R.sup.7, --CO.sub.2 R.sup.6, CONR.sup.6 R.sup.7, CH.sub.2 OR.sup.6, or CH.sub.2 NR.sup.6 R.sup.7, and R.sup.2 and R.sup.3, and R.sup.4 and R.sup.5, when attached to adjacent ring atoms, can be --(CH.sub.2).sub.3 or 4 --;in which R.sup.6 and R.sup.7 independently are hydrogen, C.sub.1 -C.sub.6 alkyl, phenyl or benzyl, and when taken together with the nitrogen to which they are attached, R.sup.6 and R.sup.7 can complete a cyclic ring having from 3 to 7 carbon atoms; ##STR2## in which R.sup.8, R.sup.8', R.sup.9, and R.sup.9' independently are hydrogen or C.sub.1 -C.sub.6 alkyl, n is 0, 1, or 2, and Z.sup..crclbar.
    Type: Grant
    Filed: March 20, 1998
    Date of Patent: December 14, 1999
    Assignee: Warner-Lambert Company
    Inventors: Joseph A. Cornicelli, Bradley D. Tait, Bharat K. Trivedi
  • Patent number: 5998463
    Abstract: This invention relates to certain 5-acyl-2-oxo-indole-3-carboxamides useful as inhibitors of glycogen phosphorylase, methods of treating glycogen phosphorylase dependent diseases or conditions with such compounds and pharmaceutical compositions comprising such compounds. This invention also relates to pharmaceutical compositions comprising those 5-acyl-2-oxo-indole-3-carboxamides in combination with antidiabetes agents and methods of treating glycogen phosphorylase dependent diseases or conditions with such compositions.
    Type: Grant
    Filed: February 16, 1999
    Date of Patent: December 7, 1999
    Assignee: Pfizer Inc
    Inventors: Bernard Hulin, Reinhard Sarges
  • Patent number: 5994388
    Abstract: The present invention relates to inhibition of angiogenesis and the treatment of diseases mediated by angiogenesis. Particularly, the invention relates to the inhibition of neovascularization and the treatment of cancer. The invention further relates to the use of cytochalasin derivatives for the inhibition of angiogenesis and the treatment of angiogenesis associated diseases. The invention also relates to new isoindolinone compounds, compositions containing them, and methods of inhibiting angiogenesis and treating angiogenesis associated diseases with the isoindolinone derivatives.
    Type: Grant
    Filed: March 17, 1998
    Date of Patent: November 30, 1999
    Assignee: The Children's Medical Center Corporation
    Inventors: Taturo Udagawa, Robert J. D'Amato, Jamshed H. Shah
  • Patent number: 5990145
    Abstract: The present invention relates to compounds of the formula I,A--B--D--E--F--G (I)in which A, B, D, E, F and G have the meanings given in the patent claims, to their preparation and to their use as medicaments. The compounds of the invention are used as vitronectin receptor antagonists and as inhibitors of bone resorption.
    Type: Grant
    Filed: December 22, 1997
    Date of Patent: November 23, 1999
    Assignees: Hoechst Aktiengesellschaft, Genentech, Inc.
    Inventors: Volkmar Wehner, Hans Ulrich Stilz, Anuschirwan Peyman, Karlheinz Scheunemann, Jean-Marie Ruxer, Denis Carniato, Jean-Michel Lefrancois, Thomas Richard Gadek, Robert McDowell
  • Patent number: 5985926
    Abstract: There is disclosed a method of preventing or delaying the occurrence of acquired immunodeficiency syndrome (AIDS) in human immunodeficiency virus (HIV) seropositive humans by administering an effective amount of a compound that inhibits cellular signaling through a specific phospholipid-based cellular signaling and signal amplification pathway. The invention further provides a method for preventing or delaying clinical symptoms of a group of viral diseases wherein the viral disease is mediated by host cell viral replication. The invention provides an advantage by attacking host cellular signaling mechanisms to prevent the development of drug resistance from rapidly mutating viruses.
    Type: Grant
    Filed: February 10, 1997
    Date of Patent: November 16, 1999
    Assignee: Cell Therapeutics, Inc.
    Inventors: David W. Leung, Gail E. Underiner, Jack W. Singer
  • Patent number: 5977130
    Abstract: The present invention is directed to an intimal hypertrophy inhibitor containing as the active ingredient an oxyindole derivative represented by the following formula (I) or a salt thereof: ##STR1## (wherein R.sup.1 represents a hydrogen atom; a phenyl group which may be substituted by a lower alkyl group, a lower alkoxy group, a lower alkylaminoalkoxy group, a hydroxy group, an amino group, a lower alkylamino group, or a halogen atom; or a pyridyl group which may be substituted by a lower alkyl group, a lower alkoxy group, a lower alkylaminoalkoxy group, a hydroxy group, an amino group, a lower alkylamino group, a halogen atom, a lower alkoxycarbonyl group, or a carboxyl group; R.sup.2 represents a phenyl group which may be substituted; or a pyridyl group which may be substituted by a lower alkyl group, a lower alkoxy group, a lower alkylaminoalkoxy group, a hydroxy group, an amino group, a lower alkylamino group, a halogen atom, a lower alkoxycarbonyl group, or a carboxyl group; R.sup.
    Type: Grant
    Filed: September 10, 1997
    Date of Patent: November 2, 1999
    Assignee: Taiho Pharmeutical Co., Ltd.
    Inventors: Atsushi Sato, Tetsuji Asao, Yuichi Hagiwara, Makoto Kitade, Yasundo Yamazaki
  • Patent number: 5972988
    Abstract: A method is disclosed for the treatment of chronic bronchitis by administering to a mammal in need thereof a therapeutically effective amount of a 1H-indole-3-glyoxylamide compound.
    Type: Grant
    Filed: March 12, 1998
    Date of Patent: October 26, 1999
    Assignee: Eli Lilly and Company
    Inventor: William Louis Macias
  • Patent number: 5948808
    Abstract: Provided in the present invention are compounds and compositions of substituted indole-3-carbinols and diindolylmethane suitable for treating estrogen-dependent tumors. Also provided are methods of treating such cancerous-conditions.
    Type: Grant
    Filed: March 7, 1997
    Date of Patent: September 7, 1999
    Assignee: The Texas A&M University System
    Inventor: Stephen H. Safe
  • Patent number: 5945413
    Abstract: This invention relates to a novel class of compounds that are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of aspartyl protease inhibitors characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting HIV-1 and HIV-2 protease activity and consequently, may be advantageously used as anti-viral agents against the HIV-1 and HIV-2 viruses. This invention also relates to methods for inhibiting aspartyl protease activity and methods for treating viral infections using the compounds and compositions of this invention.
    Type: Grant
    Filed: September 30, 1996
    Date of Patent: August 31, 1999
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Roger Dennis Tung, Francesco Gerald Salituro, David D. Deininger, Govinda Rao Bhisetti, Christopher Todd Baker, Andrew Spaltenstein
  • Patent number: 5939452
    Abstract: The invention relates to novel benzopyran and other benzo-fused leukotriene B.sub.4 (LTB.sub.4) antagonists of formula I and the pharmaceutically acceptable salts thereof, to pharmaceutical compositions containing such compounds, and to a method of using such compounds as LBT.sub.4 antagonists. The compounds of the invention inhibit the action of LTB.sub.4 and are therefore useful in the treatment of LTB.sub.4 induced illnesses such as inflammatory disorders including rheumatoid arthritis, osteoarthritis, inflammatory bowel disease, psoriasis and other skin disorders such as eczema, erythema, pruitus and acne, stroke and other forms of reperfusion injury, graft rejection, autoimmune diseases, asthma and other conditions where marked neutrophil infiltration occurs.
    Type: Grant
    Filed: April 9, 1997
    Date of Patent: August 17, 1999
    Assignee: Pfizer Inc
    Inventors: Mark Anthony Dombroski, Kevin Koch, Anthony Daniel Piscopio
  • Patent number: 5919809
    Abstract: This invention relates to novel 3-substituted-2-oxindole derivatives of the formula ##STR1## and the pharmaceutically-acceptable salts thereof which are inhibitors of prostaglandin H.sub.2 synthase, 5-lipoxygenase and interleukin-1 biosynthesis. The compounds of the invention are useful as inhibitors of prostaglandin H.sub.2 synthase and interleukin-1 biosynthesis, per se, and as analgesic, antiinflammatory and antiarthritic agents in the treatment of chronic inflammatory diseases. This invention also relates to pharmaceutical compositions comprising said 3-substituted-2-oxindole derivatives; to methods of inhibiting prostaglandin H.sub.2 synthase and biosynthesis of interleukin-1; and to treating chronic inflammatory diseases in a mammal with said compounds. Further, this invention relates to certain novel carboxylic acids useful as intermediates in the preparation of the 3-substituted-2-oxindole derivatives of this invention and to a process for the preparation of the 3-substituted-2-oxindole derivatives.
    Type: Grant
    Filed: November 4, 1993
    Date of Patent: July 6, 1999
    Assignee: Pfizer Inc.
    Inventors: Frederick J. Ehrgott, Carl J. Goddard, Gary R. Schulte
  • Patent number: 5919792
    Abstract: This invention relates to certain novel compounds and derivatives thereof, their synthesis, and their use as vitronectin receptor antagonists. The vitronectin receptor antagonist compounds of the present invention are .alpha.v.beta.3 antagonists, .alpha.v.beta.5 antagonists or dual .alpha.v.beta.3/.alpha.v.beta.5 antagonists useful for inhibiting bone resorption, treating and preventing osteoporosis, and inhibiting restenosis, diabetic retinopathy, macular degeneration, angiogenesis, atherosclerosis, inflammation and tumor growth.
    Type: Grant
    Filed: October 28, 1997
    Date of Patent: July 6, 1999
    Assignee: Merck & Co., Inc.
    Inventors: Mark E. Duggan, George D. Hartman, William F. Hoffman, Nathan C. Ihle
  • Patent number: 5919790
    Abstract: The present invention relates to compounds that are inhibitors of interleukin-1.beta. converting enzyme that have the Formula II ##STR1## This invention also relates to a method of treatment of stroke, inflammatory diseases, septic shock, reperfusion injury, Alzheimer's disease, shigellosis, and to a pharmaceutically acceptable composition that contains a compound that is an inhibitor of interleukin-1.beta. converting enzyme.
    Type: Grant
    Filed: October 2, 1997
    Date of Patent: July 6, 1999
    Assignees: Warner-Lambert Company, BASF Aktiengesellsschaft
    Inventors: Hamish John Allen, Kenneth Dale Brady, Bradley William Caprathe, Paul Galatsis, John Lodge Gilmore, Sheryl Jeanne Hays, Robert Vincent Talanian, Nigel Walker, Joseph Scott Warmus
  • Patent number: 5891902
    Abstract: The present invention relates to indole derivatives represented by formula (I): ##STR1## wherein R.sup.1 and R.sup.2 independently represent hydrogen, lower alkyl, hydroxy, lower alkoxy, halogen, --O--(CH.sub.2).sub.n --OR.sup.5, or ##STR2## R.sup.3 represents hydrogen, lower alkyl, or ##STR3## R.sup.4 represents hydroxy, lower alkoxy, substituted or unsubstituted aryloxy, or --NR.sup.10 R.sup.11, and X represents CO or SO.sub.2, with the proviso that when R.sup.3 is hydrogen or lower alkyl, and X is CO, R.sup.4 is --NR.sup.10 R.sup.11, or pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: July 15, 1996
    Date of Patent: April 6, 1999
    Assignee: Kyowa Hakko Kogyo Co., Ltd.
    Inventors: Daisuke Machii, Haruki Takai, Nobuo Kosaka, Hisakatsu Seo, Tomomi Sugiyama, Joji Nakamura, Hiroyuki Ishida, Katsushige Gomi, Soichiro Sato, Masako Uchii, Koji Suzuki
  • Patent number: 5886020
    Abstract: The present invention relates to organic molecules capable of modulating tyrosine kinase signal transduction in order to regulate, modulate and/or inhibit abnormal cell proliferation.
    Type: Grant
    Filed: June 5, 1996
    Date of Patent: March 23, 1999
    Assignee: Sugen, Inc.
    Inventors: Peng Cho Tang, Li Sun, Gerald McMahon
  • Patent number: 5883116
    Abstract: The present invention relates to organic molecules capable of modulating tyrosine kinase signal transduction in order to regulate, modulate and/or inhibit abnormal cell proliferation.
    Type: Grant
    Filed: June 5, 1996
    Date of Patent: March 16, 1999
    Assignee: Sugen, Inc.
    Inventors: Peng Cho Tang, Li Sun, Gerald McMahon
  • Patent number: 5883113
    Abstract: The present invention relates to organic molecules apable of modulating tyrosine kinase signal transduction in order to regulate, modulate and/or inhibit abnormal ell proliferation.
    Type: Grant
    Filed: June 5, 1996
    Date of Patent: March 16, 1999
    Assignee: Sugen, Inc.
    Inventors: Peng Cho Tang, Li Sun, Gerald McMahon
  • Patent number: 5880141
    Abstract: The present invention relates to organic molecules capable of modulating tyrosine kinase signal transduction in order to regulate, modulate and/or inhibit abnormal cell proliferation.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: March 9, 1999
    Assignee: Sugen, Inc.
    Inventors: Peng Cho Tang, Li Sun, Gerald McMahon
  • Patent number: 5861426
    Abstract: New compounds and their compositions having anti-inflammatory, analgesic and anti-thrombotic activities, of the general formula: A--X.sub.1 --NO.sub.2 or their salts, wherein: A is R(COX.sub.u).sub.t, wherein t is zero or 1 and u is zero or 1; and X is O, NH or NR.sub.1C wherein R.sub.1C is C.sub.1 -C.sub.10 alkyl; and R is(Ia) wherein R.sub.1 is acetoxoy, preferably n ortho-position with respect to --CO-- and R.sub.2 is hydrogen; or derivatives of acetylsalylsalicyclic acid; and X.sub.1 is --YO-- wherein Y is C.sub.1 -C.sub.20 alkylene, C.sub.5 -C.sub.7 cycloalkylene, oxy-alkyl derivatives and oxy-methyl benzyl derivatives.
    Type: Grant
    Filed: March 6, 1997
    Date of Patent: January 19, 1999
    Assignee: Nicox S.A.
    Inventors: Piero Del Soldato, Francesco Sannicolo
  • Patent number: 5859017
    Abstract: In a method for treating or preventing allergy or allergic disorders an effective amount of a compound that inhibits intracellular generation of phosphatidic acid and diacylglycerol is administered. The intracellular generation of phosphatidic acid and diacylglycerol results from allergen presentation or mast cell/basophil activation.
    Type: Grant
    Filed: April 1, 1994
    Date of Patent: January 12, 1999
    Assignee: Cell Therapeutics, Inc.
    Inventors: Elisa Eiseman, Emer Clarke, Jack W. Singer, Stuart L. Bursten
  • Patent number: 5849764
    Abstract: There are disclosed compounds of formula (I) ##STR1## and pharmaceutically acceptable salts thereof which are useful as antagonists of GnRH and as such may be useful for the treatment of a variety of sex-hormone related and other conditions in both men and women.
    Type: Grant
    Filed: December 5, 1996
    Date of Patent: December 15, 1998
    Assignee: Merck & Co., Inc.
    Inventors: Mark Goulet, Lin Chu, Thomas F. Walsh, Michael H. Fisher, Narindar N. Girotra, Matthew J. Wyvratt, Peter Lin, Wallace T. Ashton
  • Patent number: 5849710
    Abstract: The present invention relates to indol-3-ylmethylene-2-oxindole derivatives which are useful as tyrosine kinase inhibitors. The compounds are suitable for use as anti-proliferative agents, anti-metastatic agents, anti-cancer agents, and in the control of angiogenesis and in inhibiting the development of atheromatous and an immunomogulating agents.
    Type: Grant
    Filed: December 4, 1996
    Date of Patent: December 15, 1998
    Assignee: Pharmacia & Upjohn S.p.A.
    Inventors: Carlo Battistini, Dario Ballinari, Antonella Ermoli, Sergio Penco, Sergio Vioglio
  • Patent number: 5849756
    Abstract: Pharmaceutical compositions for the modulation of the immune reaction of warm blooded animals that are derivatives of the 2-oxindole-3-acetic acid or the 2-oxo-1,2,3,4-tetrahydroquinoline-4-carboxylic acid are described, and whereby the derivatives can optionally be in an equilibrium with each other.The derivatives included in the pharmaceutical compositions comprise those compounds which are already described in the literature and also new compounds.Furthermore, new derivatives of the the 2-oxindole-3-acetic acid and the 2-oxo-1,2,3,4-tetrahydroquinoline-4-carboxylic acid are described, particularly also the the pure antipodes of the mixture of enantiomeres of the 2-oxo-1,2,3,4-tetrahydroquinoline-4-carboxylic acid.
    Type: Grant
    Filed: May 26, 1995
    Date of Patent: December 15, 1998
    Assignee: Cerbios-Pharma SA
    Inventors: Ulrich Burger, Jean-Claude Jaton, Fabrizio Marazza, Ari Lewenstein, Francis M. Sirotnak
  • Patent number: 5849782
    Abstract: Methods for inhibiting a nitric oxide-mediated pathological condition and a neurodegenerative disease such as Parkinson's disease, Huntington's disease, Alzheimers's disease, and amyotrophic lateral sclerosis in a human patient, comprising administering an effective amount of a nitroindazole capable of inhibiting a neuronal nitric oxide synthase.
    Type: Grant
    Filed: July 12, 1996
    Date of Patent: December 15, 1998
    Assignee: The General Hospital Corporation
    Inventor: M. Flint Beal
  • Patent number: 5847155
    Abstract: A series of aromatic pyrrolidine derivatives and suitable pharmaceutically acceptable salts thereof are disclosed. These compounds are useful as PEP inhibitors in the treatment of Alzheimer's disease, amnesia, dementia, anxiety ischemia, or stroke.
    Type: Grant
    Filed: January 26, 1996
    Date of Patent: December 8, 1998
    Assignee: Pfizer Inc
    Inventors: W. Stephen Faraci, Arthur A. Nagel, Robin W. Spencer, Fredric J. Vinick
  • Patent number: 5840745
    Abstract: Novel hydrosoluble 3-arylidene-2-oxindole derivatives, having tyrosine kinase inhibitor activity, encompassed by general formula (I), wherein m is zero, 1 or 2; A is a bicyclic ring chosen from tetralin, naphthalene, quinoline and indole; R.sup.1 is hydrogen, C.sub.1 -C.sub.6 alkyl or C.sub.2 -C.sub.6 alkanoyl; one of R.sup.2 and R.sup.3 independently is hydrogen and the other is a substituent selected from: a C.sub.1 -C.sub.6 alkyl group substituted by 1, 2 or 3 hydroxy groups; --SO.sub.3 R.sup.4 in which R.sup.4 is hydrogen or C.sub.1 -C.sub.6 alkyl unsubstituted or substituted by 1, 2 or 3 hydroxy groups; --SO.sub.2 NHR.sup.5 in which R.sup.5 is as R.sup.4 defined above or a --(CH.sub.2).sub.n --N(C.sub.1 -C.sub.6 alkyl).sub.2 group in which n is 2 or 3; --COOR.sup.6 in which R.sup.6 is C.sub.1 -C.sub.6 alkyl unsubstituted or substituted by phenyl or by 1, 2 or 3 hydroxy groups or phenyl; --CONHR.sup.7 in which R.sup.7 is hydrogen, phenyl or C.sub.1 -C.sub.
    Type: Grant
    Filed: September 25, 1996
    Date of Patent: November 24, 1998
    Assignee: Pharmacia S. p. A.
    Inventors: Franco Buzzetti, Maria Gabriella Brasca, Antonio Longo, Dario Ballinari
  • Patent number: 5834504
    Abstract: The present invention relates to organic molecules capable of modulating tyrosine kinase signal transduction in order to regulate, modulate and/or inhibit abnormal cell proliferation.
    Type: Grant
    Filed: June 5, 1996
    Date of Patent: November 10, 1998
    Assignee: Sugen, Inc.
    Inventors: Peng Cho Tang, Li Sun, Gerald McMahon
  • Patent number: 5824677
    Abstract: Disclosed are compounds having a straight or branched aliphatic hydrocarbon structure of formula I: ##STR1## In formula I, n is an integer from one to four and m is an integer from four to twenty. Independently, R.sub.1 and R.sub.2 are hydrogen, a straight or branched chain alkyl, alkenyl or alkynyl of up to twenty carbon atoms in length or --(CH.sub.2).sub.w R.sub.5. If R.sub.1 or R.sub.2 is --(CH.sub.2).sub.w R.sub.5, w may be an integer from one to twenty and R.sub.5 may be an hydroxyl, halo, C.sub.1-8 alkoxyl group or a substituted or unsubstituted carbocycle or heterocycle. Alternatively, R.sub.1 and R.sub.2 may jointly form a substituted or unsubstituted, saturated or unsaturated heterocycle having from four to eight carbon atoms, N being a hetero atom of the resulting heterocyle. R.sub.3 may be either hydrogen or C.sub.13. In the compounds, a total sum of carbon atoms comprising R.sub.1 or R.sub.2, (CH.sub.2).sub.n and (CH.sub.2).sub.m does not exceed forty. R.sub.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: October 20, 1998
    Assignee: Cell Therapeutics, Inc.
    Inventors: J. Peter Klein, Gail E. Underiner, Anil M. Kumar
  • Patent number: 5821256
    Abstract: Novel compounds of the formula I ##STR1## in which R.sup.1, R.sup.2, R.sup.3 and X have the meaning indicated in claim 1, and their salts exhibit endothelin receptor-antagonistic properties.
    Type: Grant
    Filed: August 15, 1996
    Date of Patent: October 13, 1998
    Assignee: Merck Patent Gesellschaft mit Beschrankter Haftung
    Inventors: Dieter Dorsch, Mathias Osswald, Werner Mederski, Claudia Wilm, Claus J. Schmitges, Maria Christadler
  • Patent number: 5817690
    Abstract: A compound of the formula I: ##STR1## in which Y is hydrogen, halogen or lower alkoxy; R.sub.1 is hydrogen, lower alkyl or aryl(lower)alkyl; R.sub.2 is hydrogen, lower alkyl or --(CH.sub.2).sub.n X.sub.p Ar, where X is oxygen or carbonyl; Ar is cycloalkyl, aryl or arylaryl, oxindolyl, benzimidazolyl, indolyl, 2-oxobenzimidazolyl or 2-thioxobenzimidazolyl; or R.sub.1 and R.sub.2, taken together with the nitrogen atom to which they are attached, complete a 3,4-dihydro-1H-isoquinolinyl or 1,3-dihydro-isoindolyl; n is one of the integers 1,2,3,4,5 or 6; p is one of the integers 0 or 1; or a pharmaceutically acceptable salt thereof are inhibitors of dopamine synthesis and release, useful in the treatment of schizophrenia, Parkinson's Disease, Tourette's Syndrome, alcohol addiction, cocaine addiction, and addiction to analogous drugs.
    Type: Grant
    Filed: August 12, 1997
    Date of Patent: October 6, 1998
    Assignee: American Home Products Corporation
    Inventor: Richard Eric Mewshaw
  • Patent number: 5807883
    Abstract: Disclosed is a 2-oxoindoline derivative represented by the formula (I): ##STR1## wherein Ring A represents a benzene ring which is substituted in the 5-position or 6-position by a lower alkyl group or lower alkoxy group, R.sup.1 represents a phenyl group which is substituted by a halogen atom, a lower alkyl group or a lower alkoxy group, R.sup.2 represents a naphthyl group, indolyl group, isoquinolyl group, benzimidazolyl group or a group represented by the formula: ##STR2## wherein n represents 1 or 2, R.sup.3 represents a lower alkyl group which is substituted by a carboxyl group, a cyano group or a tetrazolyl group, O represents a single bonding arm, and Y represents a single bonding arm,or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: May 24, 1996
    Date of Patent: September 15, 1998
    Assignee: Tanabe Seiyaku Co., Ltd.
    Inventors: Koichiro Yamada, Masataka Hikota, Toshiro Shikano, Masaaki Nagasaki
  • Patent number: 5801181
    Abstract: Therapeutic compounds have the formula:(X)j--(core moiety),J being an integer from one to three, the core moiety having at least one, five- to seven-membered ring and X being a racemic mixture, R or S enantiomer, slovate, hydrate, or salt of: ##STR1## *C is a chiral carbon atom, n is an integer from one to four (preferably from one to three), one or more carbon atoms of (CH.sub.2).sub.n may be substituted by a keto or hydroxy group, and m is an integer from one to fourteen. Independently, R.sub.1 and R.sub.2 may be a hydrogen, a straight or branched chain alkane or alkene of up to twelve carbon atoms in length, or --(CH.sub.2).sub.w R.sub.5, w being an integer from two to fourteen and R.sub.5 being a mono-, di- or tri-substituted or unsubstituted aryl group, substituents on R.sub.5 being hydroxy, chloro, fluoro, bromo, or C.sub.1-6 alkoxy. Or jointly, R.sub.1 and R.sub.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: September 1, 1998
    Assignee: Cell Therapeutics, Inc.
    Inventors: John Michnick, Gail E. Underiner, J. Peter Klein, Glenn C. Rice
  • Patent number: 5795902
    Abstract: The present invention relates to a pharmaceutical preparation comprising: (A) at least one triglyceride or propylene glycol diester of fractionated coconut oil fatty acids; and (B) at least one carboxamide compound of the formula I. The composition renders the carboxamides of formula I more storage-stable and less susceptible to hydrolysis. Methods of using the composition to inhibit activation of collagenase, treating inflammatory disease, and eliciting an analgesic response are also disclosed.
    Type: Grant
    Filed: September 19, 1996
    Date of Patent: August 18, 1998
    Assignee: Pfizer Inc.
    Inventor: Imram Ahmed
  • Patent number: 5789404
    Abstract: 3-Substituted 1-arylindole compounds are provided having general formula (I) ##STR1## wherein Ar is an optionally substituted aryl group; X represents a divalent hydrocarbon group, methyleneoxy or -thioxo; R.sup.1 -R.sup.4 are hydrogen or other substituents; R.sup.5 is hydrogen, alkyl, alkenyl, etc.; R.sup.6 and R.sup.7 are independently hydrogen, alkyl, alkenyl, etc.; R.sup.8 is alkyl, alkenyl or R.sup.8 represents a group of formula 1a or 1b; wherein n is an integer from 2-8; W is O or S; U is N or CH; Z is (CH.sub.2).sub.m, m being 2 or 3, 1,2-phenylene optionally substituted with halogen or trifluoromethyl, CH.dbd.CH, COCH.sub.2 or CSCH.sub.2 ; V is O, S, CH.sub.2 or NR.sup.10, wherein R.sup.10 is hydrogen, alkyl, alkenyl, cycloalkyl, etc.; U.sup.1 is O, S, CH.sub.2 or a group NR.sup.11, wherein R.sup.11 is hydrogen, alkyl, alkenyl, etc.; and V.sup.1 is NR.sup.12 R.sup.13, OR.sup.14, SR.sup.15 or CR.sup.16 R.sup.17 R.sup.18, where R.sup.12 -R.sup.18 are as the R.sup.10 substituents; R.sup.
    Type: Grant
    Filed: August 12, 1996
    Date of Patent: August 4, 1998
    Assignee: H. Lundbeck A/S
    Inventors: Kim Andersen, Jens Kristian Perregaard
  • Patent number: 5783543
    Abstract: A carpet cleaning composition comprising: (a) a powder-form solid adsorbent; (b) rollable particles of porous material, each particle having a length greater than 1 mm, and a diameter equal to at least 10% of the length of the particle; and (c) water.
    Type: Grant
    Filed: October 30, 1996
    Date of Patent: July 21, 1998
    Assignee: Henkel Kommanditgesellschaft auf Aktien
    Inventors: Theo Fleckenstein, Alexander Ditze, Franz Kresse, Thomas Hahn
  • Patent number: 5783605
    Abstract: Cancer cells are blocked from entering differentiation pathways because of abnormal methylation enzymes, which are responsible for keeping cancer cells in cycling state. Effective differentiation inducers are those capable of acting directly or indirectly to convert abnormal methylation enzymes into normal enzymes, thereby enabling cancer cells to undergo terminal differentiation. Differentiation employing inducer alone often can not reach completion because of the damage created by the inducer. Such damage can be prevented if differentiation is induced in the presence of helper inducers, which are basically inhibitors of the component enzymes of methylation. Thus, differentiation induced in the presence of helper inducers is more likely to reach completion. Therefore, helper inducers are essential components of differentiation therapy, not just merely to potentiate the activity of differentiation inducers.
    Type: Grant
    Filed: October 15, 1996
    Date of Patent: July 21, 1998
    Inventors: Sheng-Chu Kuo, Jau-Hong Lee